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L-779450

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Chemical Structure| 303727-31-3 同义名 : Raf Kinase Inhibitor IV
CAS号 : 303727-31-3
货号 : A986611
分子式 : C20H14ClN3O
纯度 : 98%+
分子量 : 347.798
MDL号 : MFCD12828750
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(301.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 L-779450 (L-779,450) demonstrates high specificity for Raf, with p38MAPK being the only other kinase affected due to its structurally similar kinase domain to Raf. It prevents anchorage-independent growth in human tumor lines within a dosage range of 0.3 to 2 μM[2]. The impact of L-779450 (L-779,450) on TRAIL sensitivity in melanoma cell lines is characterized by high TRAIL sensitivity (A-375 and SK-Mel-147), moderate sensitivity (Mel-HO, SK-Mel-13, and SK-Mel-28), permanent resistance (MeWo, Mel-2a, and SK-Mel-103), and acquired resistance in TRAIL-selected cell lines (A-375-TS and Mel-HO-TS). Although L-779450's direct effects on apoptosis are only moderate, it significantly boosts TRAIL-induced apoptosis in TRAIL-sensitive melanoma cells and counteracts TRAIL resistance in Mel-2a, SK-Mel-103, A-375-TS, and Mel-HO-TS, achieving 16-35% apoptosis induction at 24 hours[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.38mL

2.88mL

1.44mL

28.75mL

5.75mL

2.88mL
参考文献

[1]Shelton JG, et al. Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia. 2003 Sep;17(9):1765-82.

[2]Berger A, et al. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J Invest Dermatol. 2014 Feb;134(2):430-440.